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Mol Nutr Food Res. 2012 Mar;56(3):466-74. doi: 10.1002/mnfr.201100554. Epub 2011 Dec 7.

Pharmacokinetics of xanthohumol and metabolites in rats after oral and intravenous administration.

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  • 1Linus Pauling Institute, Oregon State University, Corvallis, OR, USA.

Abstract

SCOPE:

Xanthohumol (XN), a dietary flavonoid found in hops, may have health-protective actions against cardiovascular disease and type 2 diabetes. Yet, there are limited data on the pharmacokinetics (PK) of XN. This study provides PK parameters for XN and its major metabolites in rats.

METHODS AND RESULTS:

A PK study was conducted in male jugular vein-cannulated Sprague-Dawley rats. Rats (n = 12/group) received an intravenous (IV) injection (1.86 mg/kg BW) or an oral gavage of a low (1.86 mg/kg BW), medium (5.64 mg/kg BW), or high (16.9 mg/kg BW) dose of XN. Plasma samples were analyzed for XN and its metabolites using LC-MS/MS. The maximum concentration (C(max) ) and area under the curve (AUC(0-96 h) ) of total XN (free and conjugated) were 2.9±0.1 mg/L and 2.5±0.3 h*  mg/L in IV group, 0.019±0.002 mg/L and 0.84±0.17 h*  mg/L in the oral low group, 0.043±0.002 mg/L and 1.03±0.12 h*  mg/L in the oral medium group, and 0.15±0.01 mg/L and 2.49±0.10 h*  mg/L in the oral high group.

CONCLUSION:

The bioavailability of XN is dose-dependent and approximately 0.33, 0.13, and 0.11 in rats, for the low-, medium-, and high-dose groups, respectively.

Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

PMID:
22147307
[PubMed - indexed for MEDLINE]
PMCID:
PMC3401605
Free PMC Article

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